(19) |
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(11) |
EP 0 770 602 A3 |
(12) |
EUROPEAN PATENT APPLICATION |
(88) |
Date of publication A3: |
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14.05.1997 Bulletin 1997/20 |
(43) |
Date of publication A2: |
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02.05.1997 Bulletin 1997/18 |
(22) |
Date of filing: 18.10.1996 |
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(51) |
International Patent Classification (IPC)6: C07D 211/70 |
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(84) |
Designated Contracting States: |
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AT BE CH DE DK ES FR GB GR IE IT LI NL PT SE |
(30) |
Priority: |
23.10.1995 JP 274175/95 03.10.1996 JP 263010/96
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(71) |
Applicant: Ajinomoto Co., Inc. |
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Tokyo 104 (JP) |
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(72) |
Inventors: |
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- Fujii, Akiko,
c/o Central Research Laboratories
Kawasaki-ku,Kawasaki-shi,
Kanagawa-ken (JP)
- Kubo, Mie,
c/o Central Research Laboratories
Kawasaki-ku,Kawasaki-shi,
Kanagawa-ken (JP)
- Yamamoto, Tomoya
c/o Central Research Laboratories
Kawasaki-ku,Kawasaki-shi,
Kanagawa-ken (JP)
- Shimada, Jiro
c/o Central Research Laboratories
Kawasaki-ku,Kawasaki-shi,
Kanagawa-ken (JP)
- Mihara, Ryuichi
c/o Central Research Laboratories
Kawasaki-ku,Kawasaki-shi,
Kanagawa-ken (JP)
- Naora, Hirokazu
c/o Central Research Laboratories
Kawasaki-ku,Kawasaki-shi,
Kanagawa-ken (JP)
- Asai, Koji
c/o Central Research Laboratories
Kawasaki-ku,Kawasaki-shi,
Kanagawa-ken (JP)
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(74) |
Representative: Nicholls, Kathryn Margaret et al |
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MEWBURN ELLIS
York House
23 Kingsway London WC2B 6HP London WC2B 6HP (GB) |
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(54) |
Crystals of piperidine derivatives, intermediates for production of the same, and
process for producing the same |
(57) The invention provides monohydrate and trihydrate crystals of N-(2-(4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidino)ethyl)-1-formyl-4-piperidinecarboxamide
hydrochloride. It also provides crystalline anhydride intermediates for the production
of the mono- and trihydrates.
The monohydrate and trihydrate crystals of the present invention exhibit excellent
stability. The monohydrate exhibits excellent oral absorption, and the trihydrate
exhibits a high dissolution rate, making them suitable for use in drug products to
meet various requirements.